34results about How to "Broad anti-tumor spectrum" patented technology

The present invention provides 2-hydroxy-3-amino methylene-4, 6-dibubstituted chalcone derivative with the structural general expression as shown. The preparation process includes the following steps: Lewis acid catalyzed reaction of compound I and anhydrous methy1cyanide inside inert solvent to obtain intermediate trihydroxy acetophenone amide hydrochloride; further acid hydrolysis to obtain compound II; selective etherification with alkylation reagent under alkaline cddn to obtain compound III; condensation with aromatic aldehyde under alkaline condition to obtain compound IV; and reaction with secondary amine in the presence of acid and formaldehyde to produce destination compound V. The present invention provides completely new structure compounds with powerful tumor cell inhibiting effect and IC50 value up to 0.8 micron, and capable of being used in preparing antitumor medicine.

Said invention provides tumor antigen mRNA sensitized dendritic cell tumor vaccine, preparation and use thereof, and medicinal composition of dendritic cell. Said tumor vaccine is specific mRNA modified dendritic cell vaccine which can stimulate body to produce specific immune response aiming at HER2 positive tumor, so it can be used in preventing and curing HER2 positive tumor such as breast cancer etc. said invention has high transfection efficiency, wide anti tumor gammarayspectrum and strong specificity.

The invention provides an HER2 / neu nucleic acid molecular for producing remedial vaccine for HER2 positive tumor and its applications. It includes the following elements: (a) a 7-methyl guanine cap sequence at 5'end, (b) a 110-200bp polyA tail at 3'end, (c) the coding sequences of HER2 / neu between elements (a) and (b). The said coding sequences includes multiple CTL epitopes that have been proved, do not include its PTK active domain eliminating its PTK activity, can be used for modifying dendritic cells, induce to produce specific immune response aiming at HER2 positive tumor, and can be used for preventing and treating HER2 positive tumor such as breast carcinoma. The invention also provides the said the method for constructing HER2 / neu mRNA in vitro transcription vector.

The invention discloses a substituted bismuth thiazolylalkyldithiocarbamate complex and application thereof. Six structural names of the complex are respectively bismuth thiazolylalkyldithiocarbamate, bismuth 2-methylthiazolylalkyldithiocarbamate, bismuth 2-carboxylthiazolylalkyldithiocarbamate, bismuth 2-ethoxycarbonylthiazolylalkyldithiocarbamate, bismuth S-4-carboxylthiazolylalkyldithiocarbamate and bismuth 4-ethoxycarbonylthiazolylalkyldithiocarbamate. The complex can be used for treating in-vivo diseases or symptoms of individuals, wherein the diseases or symptoms can be cancers, including human colon cancer, human mammary cancer, human myeloma, human liver cancer, human lung cancer, human leukaemia and the like. The complex has the advantages of high purity, favorable antitumor effect and broad acting strain spectrum, increases the varieties of the antineoplastic drugs, and has broad market prospects.

The invention provides a novel etoposide derivative with a hydroxamic acid structure as showed in the general formula I, a pharmaceutically-acceptable salt of the etoposide derivative, a preparation method of the etoposide derivative and usage of the etoposide derivative. In the general formula I, X is -NH-, -O-, -S-, -NH-CH2-, -O-CH2- or -S-CH2-; Y is aromatic ring, substituted aromatic ring, aromatic hyterocyclic ring or substituted aromatic hyterocyclic ring; Z is -O-, -NHCO- or -CONH-; and B is C1-C8 alkyl, C2-C8 alkenyl, alkynyl or cycloalkyl. The compound provided by the invention has good antitumor activity and can be applied clinically by oral administration, intravenous injection or intramuscular injection.

The present invention provides 2-hydroxy-3-amino methylene-4, 6-dibubstituted chalcone derivative with the structural general expression as shown. The preparation process includes the following steps: Lewis acid catalyzed reaction of compound I and anhydrous methy1cyanide inside inert solvent to obtain intermediate trihydroxy acetophenone amide hydrochloride; further acid hydrolysis to obtain compound II; selective etherification with alkylation reagent under alkaline cddn to obtain compound III; condensation with aromatic aldehyde under alkaline condition to obtain compound IV; and reaction with secondary amine in the presence of acid and formaldehyde to produce destination compound V. The present invention provides completely new structure compounds with powerful tumor cell inhibiting effect and IC50 value up to 0.8 micron, and capable of being used in preparing antitumor medicine.

The invention discloses a CIK cell, as well as a preparation method and a cell preparation thereof. The method for preparing the CIK cell comprises the following steps: placing a separated mononuclearThe invention discloses a CIK cell, as well as a preparation method and a cell preparation thereof. The method for preparing the CIK cell comprises the following steps: placing a separated mononuclearcell in a culture fluid containing phytohemagglutinin; transplanting the mononuclear cell into a culture flask enveloped by antiCD3 monoclonal antibody and antiCD28 monoclonal antibody after the cell cell in a culture fluid containing phytohemagglutinin; transplanting the mononuclear cell into a culture flask enveloped by antiCD3 monoclonal antibody and antiCD28 monoclonal antibody after the cell is cultured for 24 to 72 hours; and adding a culture fluid containing IL-1alpha and IL-2 into the culture flask to keep on culturing for 5 to 15 days, and separating the cells into different flasks tis cultured for 24 to 72 hours; and adding a culture fluid containing IL-1alpha and IL-2 into the culture flask to keep on culturing for 5 to 15 days, and separating the cells into different flasks to be cultured every 2 to 3 days. The CIK cell prepared by the method has the characteristics of obvious improved cell proliferation, great increase of CD8 cell proportion, wide antineoplastic spectrumo be cultured every 2 to 3 days. The CIK cell prepared by the method has the characteristics of obvious improved cell proliferation, great increase of CD8 cell proportion, wide antineoplastic spectrum and strengthened antineoplastic activity. The CIK cell and the cell preparation can effectively prevent the metastasis and the recrudescence for of postoperative patients with tumor, can be combinedand strengthened antineoplastic activity. The CIK cell and the cell preparation can effectively prevent the metastasis and the recrudescence for of postoperative patients with tumor, can be combinedwith chemicotherapy to effectively reduce toxic and side effects of the chemicotherapy, strengthens the survivability tolerance of the patients to improve healing efficacy, and can obviously prolong lwith chemicotherapy to effectively reduce toxic and side effects of the chemicotherapy, strengthens the survivability tolerance of the patients to improve healing efficacy, and can obviously prolong lifecycle to of end-stage patients so as to improve the life living quality.ifecycle to of end-stage patients so as to improve the life living quality.

The invention discloses water-soluble camptothecine derivatives with its general formula being (I), its mono-isomer, antimer and relevant mixer, medical-use salt and active metabolism. The definition of R1 and R2 is expressed in instruction manual. The derivatives are prepared through Sonogashira reaction with 7- chloro- camptothecine by using palladium catalyst with existance of organophosphorus ligand and alkali. Said water-soluble camptothecine derivatives can resist tumor and can be used to prepare anti-tumor medicine.

The invention discloses a novel hopane-type triterpene compound with 2 and 3 breaks which is rarely seen in natural products at present, and the molecular formula is C30H48O3. The compound may be derived from the Latin name Megacodon? stylophorus? (C.? B.? Clarke)? H.? Smith's plants. The chemical structure and three-dimensional configuration of the compound were confirmed by the comprehensive analysis of two-dimensional nuclear magnetic resonance spectrum and X-ray diffraction. At the same time, the invention also discloses a preparation method of the compound. In addition, the anti-tumor test in vitro shows that the compound has obvious inhibitory effect on more than ten kinds of tumor cell lines. The invention provides a new lead compound for the development of new antitumor drugs, and is of great significance to the development and utilization of Tibetan medicine resources in my country.

The invention discloses an F3 polypeptide targeted nano organic metal frame material (nMOFs) and a preparation method thereof. A transition element Zr and an organic ligand BDC-N3 are synthesized intoa nano-carrier UIO-66-N3, and then two PEGs of which the tail ends are modified by alkynyl are loaded on the surface of the UIO-66-N3 through a click chemical reaction, thereby avoiding the aggregation between nanoparticles, and increasing the long circulation effect of the nanoparticles; then an F3 polypeptide is conjugated on the surface of the UIO-66-N3 to give the UIO-66-N3 targeting. In thewhole chemical transformation process, the structure of a framework of the UIO-66-N3 is retained and loaded with DOX to prepare a fluorescent imaging agent for treatment, and the nanoparticles of thesynthesized DOX / UIO-66-PEG-F3 have the effects of treatment and targeting. The F3 polypeptide targeted nano organic metal frame material (nMOFs) has potential clinical application value, and providesmore powerful technical support for the treatment of malignant tumors.

The invention provides a colchicine derivative that is shown as general formula I and contains histone deacetylase inhibitory activity, its pharmaceutically acceptable salts, a preparation method and application thereof. In the general formula I, X can be carbonyl, methylene, substituted methylene, ethylidene and substituted ethylidene; Y can be an aromatic ring, a substituted aromatic ring, a heteroaromatic ring and a substituted heteroaromatic ring; and Z can be hydrogen, an aromatic ring, a substituted aromatic ring, a heteroaromatic ring and a substituted heteroaromatic ring. The compounds have good anti-tumor activity, and can be applied by means of oral administration, intravenous injection, intramuscular injection and the like clinically.

The invention discloses a benzimidazole pyridine complex and a method for preparing the same. The method is that Pb(NO3)2, 2, 6-bisbenzimidazole pyridine (bbp) and 5-nitroisophthalicacid (nipa) are proportionally weighed according to the molar ratio of 1:1:(1-0.5) to be put into a container and are added with water to be stirred for 10-15 minutes; then, the stirred raw material liquid is poured into a reactor, the reactor is covered to be heated to 160-165 DEG C, and then, thermal insulation reaction is carried out for 115-120 hours; and a gradient heating method is adopted to cool the raw material liquid to room temperature so as to obtain a colorless blocky crystal complex, i.e. the benzimidazole pyridine complex [Pb2(nipa) (Hbbp)2]n.nH2O is obtained. The benzimidazole pyridine complex has the characteristics of good stability and obvious functions in inhibiting three types of human cancer cells of human breast cancer cells, lung cancer cells and cervical cancer cells, and provides guidance for the research and development of an anticancer complex.

The invention provides an HER2 / neu nucleic acid molecular for producing remedial vaccine for HER2 positive tumor and its applications. It includes the following elements: (a) a 7-methyl guanine cap sequence at 5'end, (b) a 110-200bp polyA tail at 3'end, (c) the coding sequences of HER2 / neu between elements (a) and (b). The said coding sequences includes multiple CTL epitopes that have been proved, do not include its PTK active domain eliminating its PTK activity, can be used for modifying dendritic cells, induce to produce specific immune response aiming at HER2 positive tumor, and can be used for preventing and treating HER2 positive tumor such as breast carcinoma. The invention also provides the said the method for constructing HER2 / neu mRNA in vitro transcription vector.

This invention discloses a novel natural anti-tumor compound with novel molecular frame and high anti-tumor activity. The novel natural anti-tumor compound is derived from waxmyrtle. This invention also discloses its preparation method. The method comprises: lixiviating waxmyrtle coarse powder, vacuum-concentrating, dispersing in water, extracting with an appropriate organic solvent, separating, and purifying to obtain the compound. The compound has wide applications in anti-tumor drugs.